Methods and compositions for the treatment of retinal, neurological and other related diseases

Abstract

The present invention provides compositions and formulations of biologically active compounds complexed with a solid lipid particle which is able to traverse the blood-retinal barrier and treat retinal and neurological diseases.

1 . A method of treating, reducing or inhibiting retinal inflammation in a subject, the method comprising:
 administering an effective amount of an enhanced oral bioavailable formulation of curcumin, lutein or a combination thereof, the enhanced oral bioavailable formulation comprising:   (a) curcumin, lutein or a combination thereof complexed with a solid lipid particle;   (b) a carrier granule comprising an agglomeration of the solid lipid particle embedded in, adhered to or both embedded in and adhered to, the carrier granule, wherein the solid lipid particle carrier granule complex is formulated for oral dosing.   
     
     
         2 . A method of treating a retinal disease in a subject, the method comprising:
 administering an effective amount of an enhanced oral bioavailable formulation of curcumin, lutein or a combination thereof, the enhanced oral bioavailable formulation comprising:   (a) curcumin, lutein or a combination thereof complexed with a solid lipid particle;   (b) a carrier granule comprising an agglomeration of the solid lipid particle embedded in, adhered to or both embedded in and adhered to, the carrier granule, wherein the solid lipid particle carrier granule complex is formulated for oral dosing.   
     
     
         3 . The method of  claim 2 , wherein the retinal disease is selected from the group consisting of glaucoma, diabetic retinopathy, and retinal vein occlusion. 
     
     
         4 . The method of  claim 2 , wherein the retinal disease is associated with retinal inflammation. 
     
     
         5 . The method of  claim 1 , wherein the carrier granule has a particle size from about 150 to about 840 microns. 
     
     
         6 . The method of  claim 1 , wherein the solid lipid particle has a particle size from about 5 to about 20 microns. 
     
     
         7 . The method of  claim 1 , wherein the solid lipid particle comprises one or more long-chain lipid. 
     
     
         8 . The method of  claim 1 , wherein the solid lipid particle comprises one or more long chain lipid selected from the group consisting of soy lecithin, phosphatidylcholine, stearic acid, and ascorbyl palmitate. 
     
     
         9 . The method of  claim 1 , wherein the solid lipid particle comprises dextrin, silicone dioxide, or both. 
     
     
         10 . The method of  claim 1 , wherein the ratio steric acid:phosphatidylcholine is in a range of about 1.25:1 to about 3.5:1. 
     
     
         11 . The method of  claim 1 , wherein the solid lipid particle comprises a core comprising the active ingredient, phosphatidylcholine and ascorbyl palmitate, and a coating of stearic acid. 
     
     
         12 . The method of  claim 1 , wherein the solid lipid particle is embedded in the carrier granule. 
     
     
         13 . The method of  claim 1 , wherein the solid lipid particle is adhered to the surface of the carrier granule. 
     
     
         14 . The method of  claim 1 , wherein the solid lipid particle is encased within the carrier granule. 
     
     
         15 . The method of  claim 1 , wherein the carrier granule is formed in all or in part from fractured solid lipid microparticles. 
     
     
         16 . The method of  claim 1 , wherein at least one of the carrier granule, solid lipid particle, and solid lipid particle carrier granule complex pass through the blood-ocular barrier. 
     
     
         17 . The method of  claim 1 , wherein the formulation comprises:
 about 15 to about 40% of curcumin, lutein, or a combination thereof;   about 7 to about 25% soya lecithin;   about 7 to about 30% maltodextrin;   about 1 to about 3% ascorbyl palmitate; and   about 0.3 to about 2% silicone dioxide.   
     
     
         18 . The method of  claim 17 , wherein the soya lecithin is phosphatidylcholine. 
     
     
         19 . The method of  claim 1 , wherein the formulation comprises:
 about 10 to about 30% of curcumin, lutein, or a combination thereof;   about 10 to about 20% of phosphatidylcholine;   about 25 to about 35% stearic acid;   about 25 to about 40% dextrin;   about 1 to about 4% ascorbyl palmitate; and   about 0.1 to about 3% silicon dioxide.